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РЖ ВИНИТИ 34 (BI48) 96.06-04Т2.396

Synthesis and biological evaluation of N{6}-cycloalkyl derivatives of 1-deazaadenine nucleosides: A new class of anti-human immunodeficiency virus agents [Text] / Gloria Cristalli [et al.] // J. Med. Chem. - 1995. - Vol. 38, N 20. - P4019-4025 . - ISSN 0022-2623
Перевод заглавия: Синтез и оценка биологической активности N{6}-циклоалкильных производных 1-дезазаадениновых нуклеозидов: новый класс соединений, активных против ВИЧ
Аннотация: The present study was aimed at direct comparison of the activity as anti-HIV-1 (human immunodeficiency virus) and anti-HSV-1 (herpes simplex virus type-1) agents and ADA (adenosine deaminase) inhibitors of a series of 1-deazapurine nucleosides with the N{6} nitrogen unsubstituted or bearing methyl or cycloalkyl substituents, with or without a chloro group in the 2-position, and with the glycosylic moiety being ribose (1-16), 2'-deoxyribose (17-32), or 2',3'-dideoxyribose (33-48). Nucleosides bearing cycloalkyl substituents on N{6} exhibited moderate to good anti-HIV-I activity, compared to 2',3'-dideoxyadenosine, with the degree and pattern of improvement depending on the structure of the sugar moiety. In general, 2'-deexy- and 2',3'-dideoxy derivatives were more potent compounds than the corresponding ribose nucleosides. Compounds bearing a 6-cycloheptyl or cyclooctylamine were the most active in every series. The presence of a chloro group in the 2-position improved both activity and therapeutic index in every series, the most active compound being 2'-deoxy-2-chloro-N{6}-cycloheptyl-1-deazaadenosine (23; ED[50]=0.2 'мю'M). On the other hand, most of these derivatives were inactive as anti-HSV-1 agents, showing a high degree of virus selectivity. The 1-deazaadenine derivatives were not substrates of adenosine deaminase, and some of them proved to be good inhibitors of the enzyme. Италия, Dipart. di Scienze Chimiche, Univ. di Camerino, 62032 Camerino. Библ. 31

ГРНТИ	34.45.21

ВИНИТИ 341.45.21.95.47.17
Рубрики: ПРОТИВОВИРУСНЫЕ СРЕДСТВА
ЦИКЛОАЛКИЛЬНЫЕ* N6-ПРОИЗВОДНЫЕ
ДЕАЗААДЕНИНОВЫЕ* 1-НУКЛЕОЗИДЫ
СИНТЕЗ
СТРУКТУРА-АКТИВНОСТЬ
ВИЧ-1
ИНГИБИРОВАНИЕ АДЕНОЗИНДЕЗАМИНАЗЫ
ЦИТОТОКСИЧНОСТЬ
IN VITRO

Доп.точки доступа:
Cristalli, Gloria; Vittori, Sauro; Eleuteri, Alessandra; Volpini, Rosaria; Camaioni, Emidio; Lupidi, Giulio; Mahmood, Naheed; Bevilacqua, Francesca; Palu, Giorgio

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